• 제목/요약/키워드: Inhibitory Activity

검색결과 7,150건 처리시간 0.03초

상심자의 모노아민산화효소 저해활성 (The Inhibitory Activity on Monoamine Oxidase of the Fruit of Morus alba)

  • 황금희;송임
    • 생약학회지
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    • 제34권2호통권133호
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    • pp.185-189
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    • 2003
  • We examined the inhibitory activities against monoamine oxidase (MAO) of Morus alba in vitro and in vivo methods. Methanolic extract of M. alba showed significantly inhibitory activities on MAO-A and MAO-B that were prepared from rat brain and liver in vitro. The inhibitory activities were measured by serotonin and benzylamine as substrates, respectively. MAO-A and MAO-B activities were potently inhibited by ethylacetate extracts of M. alba in vitro tests. Those activities in vivo tests have different tendency each other. MAO-A activity was increased by the oral administration of methanolic extract of M. Alba, while, MAO-B activity was decreased. Consequently, we can suggest that M. alba may have the effects on the inhibitory activities against MAO both in vitro and in vivo.

Effect of 2-NBDG, a Fluorescent Derivative of Glucose, on Microbial Cell Growth

  • Shin, Dong-Sun;Oh, Ki-Bong
    • Journal of Microbiology and Biotechnology
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    • 제12권5호
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    • pp.834-837
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    • 2002
  • A fluorescent glucose analogue,2-[N-(7-nitrobenz-2-ox a-1,3-diazol-4-yl) amino] -2- deoxy-D-glucose (2-NBDG), which had previously been developed for the analysis of glucose uptake in living cells, was investigated to determine its biological activity on microorganisms.2-NBDG did not show any inhibitory effect on growth of yeast cells and bacteria. In contrast, 2-NBDG exhibited strong inhibitory effects on filamentous fungal growth. The growth of filamentous fungi was completely inhibited, when 2-NBDG was supplemented as sole carbon source. The inhibitory effect was decreased by the addition of glucose in the test medium. Furthermore, 2-NBDC inhibited chitinase activity of Trichoderma sp. These results suggested that the inhibitory effects of 2-NBDG on filamentous fungi might be partially due to the inhibition of chitinase.

Isolation of 3-Galloylprocyanidin B3, a Glucosyltransferase Inhibitor from the Korean Green Tea Leaves

  • Cho, Young-Je
    • Journal of Applied Biological Chemistry
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    • 제43권4호
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    • pp.273-276
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    • 2000
  • In the course of surveying the anti-plaque agents for dental caries prevention, the extract of Korean green tea leaves (KGTL) was tested for inhibitory activity against Streptococcus mutans adhering to glass surfaces in the presence of crude glucosyltransferase (GTase). The extracts of KGTL showed a positive inhibitory activity against GTase. The active compound was purified through Sephadex LH-20 and MCI gel CHP-20P columns. A positive reaction was shown in the anisaldehyde-$H_2SO_4$ test, which confirmed the condensed tannin. The inhibitory compound was identified as 3-galloylprocyanidin $B_3$ through IR, negative FAB-mass, and $^{1}H$-NMR spectroscopic analyses. Acetone extract and 3- galloylprocyanidin $B_3$ of KGTL showed inhibitory effect against GTase. The percent of inhibition was determinated to be 71.84% (P<0.01) with 10 mM 3-galloylprocyanidin B3. The 3-galloylprocyanidin $B_3$, which possessed a galloyl, showed a higher inhibitory activity against glucosyltransferase than monomeric (+)-catechin and procyanidine $B_3$ which had no galloyl group.

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Development of Novel Small Chemical Inhibitors for Lck SH Domain with in vitro T-cell Inhibitory Activity

  • Park, See-Hyoung;Kang, Mi-Ae;Shim, Hyeong-Soo;Cho, Hyeong-Jin;Won, Jong-Hwa;Lee, Keun-Hyeung
    • Bulletin of the Korean Chemical Society
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    • 제27권9호
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    • pp.1353-1358
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    • 2006
  • We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

Extraction and Characteristics of Anti-obesity Lipase Inhibitor from Phellinus linteus

  • Lee, Jong-Kug;Jang, Jeong-Hoon;Lee, Jong-Tae;Lee, Jong-Soo
    • Mycobiology
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    • 제38권1호
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    • pp.52-57
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    • 2010
  • To develop a potent anti-obesity lipase inhibitor from mushroom, the lipase inhibitory activities of various mushroom extracts were determined. Methanol extracts from Phellinus linteus fruiting body exhibited the highest lipase inhibitory activity (72.8%). The inhibitor was maximally extracted by treatment of a P. linteus fruiting body with 80% methanol at $40^{\circ}C$ for 24 hr. After partial purification by systematic solvent extraction, the inhibitor was stable in the range of $40\sim80^{\circ}C$ and pH 2.0~9.0. In addition to lipase inhibitory activity, the inhibitor showed 59.4% of superoxide dismutase-like activity and 56.3% of acetylcholinesterase inhibitory activity.

종대황 스틸벤 유도체의 Cyclooxygenase 저해작용 (Inhibitory Effects of Stilbene Derivatives from Rheum undulatum on Cyclooxygenase Activity)

  • 이충렬;이학성;김현;백구현;토쿠오카 키요시;정성현;고성권
    • 생약학회지
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    • 제34권1호통권132호
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    • pp.25-27
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    • 2003
  • In order to clarify the anti-thrombosis activity of rhubarb, we investigated the effect of stilbene derivatives from rhizomes of Rheum undulatun on cyclooxygenase activity. Stilbene derivatives (desoxyrhapontigenin, rhapontigenin, piceatannol) exhibited the inhibitory effects on COX-1, and desoxyrhapontigenin showed inhibitory effect on COX-2. These inhibitory effect may partially contributed to anti-thrombosis activity of rhubarb.

Acetylcholinesterase Inhibitors from the Stem of Zea mays

  • Sim, Jae Young;Kim, Mi Ae;Kim, Myong Jo;Chun, Wanjoo;Kwon, Yongsoo
    • Natural Product Sciences
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    • 제20권1호
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    • pp.13-16
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    • 2014
  • Five compounds were isolated from the stem of Zea mays. Based on spectral data, they were identified as 4-hydroxybenzaldehyde (1), N-trans-p-coumaryl tyramine (2), N-trans-ferulyl tryptamine (3), N-(p-coumaryl) serotonine (4), and N-(p-coumaryl)-tryptamine (5). All isolates were evaluated in vitro for their inhibitory activity on acetylcholinesterase. Among tested compounds, compounds 2 - 5 exhibited acetylcholinesterase inhibitory activity, with $IC_{50}$ values of 125, 60.4, 183.5 and 53.3 ${\mu}M$, respectively. Compound 1 did not show acetylcholinesterase inhibitory activity in the present study.

Fractionation and Angiotensin I-converting Enzyme (ACE) Inhibitory Activity of Gelatin Hydrolysates from by-products of Alaska Pollock Surimi

  • Park, Chan-Ho;Kim, Hyung-Jun;Kang, Kyung-Tae;Park, Jae-W.;Kim, Jin-Soo
    • Fisheries and Aquatic Sciences
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    • 제12권2호
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    • pp.79-85
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    • 2009
  • Gelatin hydrolysates with a high inhibitory activity against angiotensin I-converting enzyme (ACE) were fractionated from Alaska pollock surimi refiner discharge. The ACE-inhibitory activity, expressed as $IC_{50}$ (mg/mL), was highest (0.49 mg/mL) in gelatin hydrolysates formed by sequential 2-hr treatments of Pronase and Flavourzyme. After fractionation through four different membrane filters with molecular weight cut-offs of 3, 5, 10, and 30 kDa, the highest ACE-inhibitory activity (0.21 mg/mL) was observed with the 3-kDa filtrate.

Structural Requirement of Isoflavonones for the Inhibitory Activity of Interleukin-5

  • Cho, Soo-Hyun;Lee, Jee-Hyun;Dang, The-Hung;Ju, Jung-Hun;Kim, Mi-Kyung;Lee, Seung-Ho;Ryu, Jae-Chun;Kim, Young-Soo;Jung, Sang-Hun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.354.3-355
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    • 2002
  • Interleukin (IL)-5 appears to be one of the main proinflammatory mediators among a growing number of cytokines and chemokines that induce eosinophilic inflammation. Sophoricoside and their analogs isolated from Sophora japonica show relatively potent inhibitory activity of interleukin (IL)-5 as a small molecule. To identify structural requirements of this isoflavonone for its inhibitory activity against IL -5. isoflavonones. isoflavanones, and their glycosides were prepared and tested their inhibitory activity against IL-5. (omitted)

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한약재의 최종당화산물 생성저해활성 검색 (Screening of Korea Traditional Herbal Medicines with Inhibitory Activity on Advanced Glycation End Products (AGEs) Formation)

  • 장대식;이윤미;김영숙;김진숙
    • 생약학회지
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    • 제37권1호통권144호
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    • pp.48-52
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    • 2006
  • Advanced glycation end products (AGEs) are largely involved in the pathogenesis of diabetic complications. As part of our ongoing project directed toward the discovery of preventive and/or delay agents for diabetic complications from natural sources, 92 Korean traditional herbal medicines have been investigated with an in vitro evaluation system using AGEs inhibitory activity. Of these, 17 herbal medicines exhibited a significant inhibitory activity against AGEs formation. Particularly, 9 herbal medicines, i.e., Cinnamomi Cortex, Artemisiae Argyi Herba, Ammoni Tsao-ko Fructus, Menthae Herba, Amomi Semen, Polygoni Avicularis Herba, Lycopi Herba, Salviae Radix, and Nelumbinis Semen showed more potent inhibitory activity (2-4 fold) than the positive control aminoguanidine.